CAY10746

CAY10746 is a selective Rho kinase (ROCK) inhibitor. CAY10746 has inhibitory activity for ROCK I, ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be used for the research of diabetic retinopathy (DR)[1].

Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK

Research Areas >> Metabolic Disease

Signaling Pathways >> Stem Cell/Wnt >> ROCK

Signaling Pathways >> TGF-beta/Smad >> ROCK

IC50: 0.014 μM (ROCK I); 0.003 μM (ROCK II)[1]

CAY10746 (compound 12j) 对 ROCK I、ROCK II 具有抑制活性，IC50 值分别为 0.014 μM 和 0.003 μM[1]。 CAY10746（0.1、1 和 10 μM；0.25、1、2 和 4 h）抑制 SH-SY5Y 细胞中的 ROCK 激酶活性[1]。 CAY10746（1 μM；24 h、36 h）在体外抑制内皮细胞迁移[1]。 CAY10746（1 μM；5 days）保护视网膜神经元免受高葡萄糖诱导的氧化应激和细胞凋亡介导的细胞死亡[1]。 CAY10746（1 μM；5 days）抑制 Müller 细胞的不当增殖并促进在高糖微环境中培养的视网膜外植体中的血管退化[1]。 Western Blot Analysis[1] Cell Line: SH-SY5Y cells Concentration: 0.1, 1 and 10 μM; 10 μM Incubation Time: 2 h; 0.25, 1, 2 and 4 h Result: Inhibited the phosphorylation of MYPT1 but did not impact the MYPT1 expression in dose-dependence and time- dependence. Cell Proliferation Assay[1] Cell Line: SH-SY5Y cells Concentration: 1 μM Incubation Time: 5 days Result: Significantly protected the cells from death. Cell Migration Assay [1] Cell Line: HUVEC cells Concentration: 1 μM Incubation Time: 24 h, 36 h Result: Significantly reduced migrating cell numbers and significantly reduce the rate of wound healing at 24 h and 36 h. Apoptosis Analysis[1] Cell Line: ex vivo DR model Concentration: 1 μM Incubation Time: 5 days Result: Significantly protected neuronal cells from death.

[1]. Lanying Zhao, et al. Discovery of 4 H-Chromen-4-one Derivatives as a New Class of Selective Rho Kinase (ROCK) Inhibitors, which Showed Potent Activity in ex Vivo Diabetic Retinopathy Models. J Med Chem. 2019 Dec 12;62(23):10691-10710.